Sitagliptin Research Paper

Sitagliptin is a drug that has proven its effectiveness towards managing type 2 diabetes. Type 2 diabetes is a progressive disease characterized by relative lack of insulin. It consists of insulin resistance as well as dysfunction of β-cells. Insulin resistance indicates that more insulin is required for normal body functioning along with decreased insulin concentration at all levels.4 This lowers the glucose transporter action associated with insulin deficiency.4 Malfunctioning of pancreatic β-cells, which causes impaired production of insulin, is another factor present in type 2 diabetes. Sitagliptin is a highly selective DPP-4 inhibitor; it exerts its actions in patients diagnosed with type 2 diabetes by decelerating inactivation of incretin hormones and thus prolonging their actions.3 The function of incretin hormones, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), is to regulate the glucose homeostasis.3 Incretin hormones are released during fasting state.3 After consumption of foods, activation of these hormones promotes insulin production and insulin release from pancreatic β-cells.3 The DPP-4 enzyme rapidly degrades these incretin hormones and causes the decrease of insulin in patients diagnosed with type 2 diabetes.3 Sitagliptin selectively inhibits the DPP-4 …show more content…
CYP3A4 is predominantly found in the liver, however it is also present in other organs and tissues of the body, allowing for greater active sites.2 Therefore no alternations to the metabolism process are needed. Elimination of Sitagliptin occurs primarily through renal excretion, involving active tubular secretion.3 Lowering dosages are recommended in patients with moderate and severe renal insufficiency; Sitagliptin is primarily eliminated unchanged via renal excretion, thus dosage adjustments are required for patients with moderate to severe renal